Tripterygium Wilfordii Hook f(Lei Gong Teng) is a kind of vine plant of the Celastraceae family, and mainly grows under humid conditions near the forest in the Yangtze River basin and southeast area of China. Its major chemical components include diterepenes, triterpenes, sesquiterpenes, alkaloids and so on. Pharmacological studies conducted in the last twenty years demonstrated that the extract of Tripterygium Wilfordii Hook f has anti-flammable, immunosuppressive, male sterile, anti-tumor and antibacterial activities. One diterpenoid lactone in Tripterygium Wilfordii Hook f, triptolide (shown below), was found to have significant biological activity, especially in respect to its inhibiting immune function.
However, the high toxicity of triptolide limited its clinic uses, and after studying the structure-activity relationship of triptolide thoroughly, the present inventors designed and synthesized a series of novel triptolide derivatives through chemical modification on structure moiety of this lead compound to complete the present invention.
Therefore, the present invention provides highly bioactive triptolide derivatives with low toxicity.
The present invention also provides the application of triptolide derivatives in preparing anti-flammable agents, immunosuppressant agents and other pharmaceutical compositions used in treating related diseases.